Enzyme kinetic parameters for metabolism of CJ-12,458 in pooled human liver microsomes
| Parameter | CP-611,781 (Diol) | CP-616,762 (1° OH) |
|---|---|---|
| K Mapp (1) (μM) | 5.4 | 8.5 |
| V max (1) (pmol/min/mg) | 37 | 19 |
| CL′int (1) (μl/min/mg) | 6.9 | 2.2 |
| CL′int (2) (μl/min/mg) | 0.23 | 0.10 |
| Total CL′int (μl/min/mg) | 7.1 | 2.3 |
| Scaled CL′int(ml/min/kg)1-a | 6.4 | 2.1 |
↵1-a Intrinsic clearance scaled per kilogram of body weight using the values of 45 mg of microsomal protein per g of liver and 20 g of liver per kg of body weight in humans.